New chromanone derivatives containing thiazoles: Synthesis and antitumor activity evaluation on A549 lung cancer cell line

Abstract

Novel 2‐[2‐(chroman‐4‐ylidene)hydrazinyl]‐4/5‐substituted thiazole derivatives (2a–i) were synthesized and investigated for their anticancer activity. Cytotoxic activity on A549 and NIH/3T3 cell lines was determined, most of the compounds exhibited high cytotoxic profile with selectivity. Selected compounds 2b, 2c, 2e, 2g, 2h, and 2i were tested to determine induction of apoptosis, mitochondrial membrane depolarization, and cell cycle arrest. The results showed that the compounds induced apoptosis intrinsically that they triggered loss of mitochondrial potential through increasing the accumulation of cells in G2/M. Besides, intrinsic apoptotic pathway was supported by down‐regulation of anti‐apoptotic protein Bcl‐2 and up‐regulation of proapoptotic protein Bax. Molecular docking study for compounds 2b, 2c, and 2g was promoted experimental outcomes.

Synthesis, density functional theory calculation, molecular docking studies, and evaluation of novel 5‐nitrothiophene derivatives for anticancer activity

“…[ 57 ] The MTT assay for cytotoxicity of compounds has been determined according to the previously published procedures. [ 43 ]…”

“…The analysis of mitochondrial membrane potential by flow cytometry for compounds 2a–2d , and cisplatin has been determined according to the previously published procedures. [ 43 ]…”

“…[ 41 ] In many of our previous studies, the anticancer effects of thiazole derivatives were determined especially on lung cancer. [ 42–44 ]…”

“…[41] In many of our previous studies, the anticancer effects of thiazole derivatives were determined especially on lung cancer. [42][43][44] Based on the promising aspects indicated above, the method of this study comprises the bioactive substances thiazole and for the aim of synergism, and the synthesized compounds were tested as anticancer agents. In this study, we synthesized the compounds 2a-2j and investigated their anticancer activity against A549 human lung carcinoma and L929 murine fibroblast cell lines.…”

Antimicrobial Activity and DFT Studies of a Novel Set of Spiropyrrolidines Tethered with Thiochroman-4-one/Chroman-4-one Scaffolds

“…They are used as versatile intermediates for the synthesis of many natural products [14][15][16][17][18][19] and constitute interesting building blocks in drug design and organic synthesis [20][21][22][23]. They also exhibit significant biological activities allowing their use as anticancer [24][25][26][27], antifungal and antibacterial [28][29][30][31], anti-inflammatory [32,33], antidiabetic [34,35], anti-leishmanial (caused by protozoan parasites) [36,37], and insecticidal agents [38] (Figure 1).…”